The challenge of developing green tea polyphenols as therapeutic agents.
The challenge of developing green tea polyphenols as therapeutic agents.
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DOI：
10.1007/s10787-008-8031-x
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发表时间：
2008-10
影响因子：
5.8
通讯作者：
Chan, T. H.
中科院分区：
文献类型：
--
作者：
Huo, C.;Wan, S. B.;Lam, W. H.;Li, L.;Wang, Z.;Landis-Piwowar, K. R.;Chen, D.;Dou, Q. P.;Chan, T. H.
绿茶及其主要成分(-)-表没食子儿茶素没食子酸酯[(-)- egcg]的健康益处已得到流行病学、细胞培养、动物和临床研究结果的广泛支持。另一方面，绿茶多酚类药物在生理条件下的稳定性、生物利用度和代谢转化等方面还面临着许多问题。我们之前报道过(-)- egcg的合成过乙酸酯比(-)- egcg本身具有更高的稳定性和更好的生物利用度，并且在体外和体内条件下都可以作为前药。儿茶素的类似物已被合成，它们的构效关系为蛋白酶体抑制机制的研究提供了新的思路。儿茶素的代谢性甲基化导致甲基化(-)- egcg可能改变这些化合物的生物活性。
The health benefits of green tea and its main constituent (-)-epigallocatechin gallate [(-)-EGCG] have been widely supported by results from epidemiological, cell culture, animal and clinical studies. On the other hand, there are a number of issues, such as stability, bioavailability and metabolic transformations under physiological conditions, facing the development of green tea polyphenols into therapeutic agents. We previously reported that the synthetic peracetate of (-)-EGCG has improved stability and better bioavailability than (-)-EGCG itself and can act as pro-drug under both in vitro and in vivo conditions. Analogs of catechins have been synthesized and their structure activity relationship provides an understanding to the mechanism of proteasome inhibition. Metabolic methylation of catechins leading to methylated (-)-EGCG may alter the biological activities of these compounds.
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影响因子：
5.2
作者：
Li, LH;Chan, TH
通讯作者：
Chan, TH
影响因子：
3.5
作者：
Lam, WH;Kazi, A;Chan, TH
通讯作者：
Chan, TH
影响因子：
5.6
作者：
Landis-Piwowar, Kristin R.;Wan, Sheng Biao;Dou, Q. Ping
通讯作者：
Dou, Q. Ping
影响因子：
2.9
作者：
Gensler, HL;Timmermann, BN;Alberts, DS
通讯作者：
Alberts, DS
影响因子：
6.2
作者：
Jatoi, A;Ellison, N;Flynn, PJ
通讯作者：
Flynn, PJ